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[【学科前沿】] Screening of 5-HT1A Receptor Antagonists using Molecularly Imprinted Polymers

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发表于 2007-4-24 19:46:50 | 显示全部楼层 |阅读模式
Title:Screening of 5-HT1A Receptor Antagonists using Molecularly Imprinted Polymers
標題:分子印跡聚合物篩選5-羥色胺受體拮抗劑
Author:Naphtali A. O'Connor, David A. Paisner, Donna Huryn, and Kenneth J. Shea
作者:Naphtali A. O'Connor, David A. Paisner, Donna Huryn, and Kenneth J. Shea
Resource: JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2007,129 (6):1680 -1689.
文章来源:美国化学杂志, 2007,129 (6):1680 -1689.
Abstract:Molecular imprinting produces network polymers with recognition sites for imprint molecules.
摘要:
分子印记技术可以生产带有印迹分子识别位点的网状聚合物。
The high binding affinity and selectivity in conjunction with the polymers' physical robustness positions molecular imprinted polymers (MIPs) as candidates for use as preliminary screens in drug discovery.
做为初步筛选新药的方法,当与聚合物物理骨架中放置的分子印迹聚合物(MIPs)相结合时会有高亲和力和高选择性。

As such, MIPs can serve as crude mimics of native receptors. In an effort to evaluate the relationship between MIPs and native receptors, imprinted polymers for WAY-100635, an antagonist of the serotonin (5-HT) receptor subtype 5-HT1A were prepared.
如此,MIPs可以做为自然受体的相似物。在试图评估MIPs和自然受体间关系时,一种5-羟色胺(5-HT)受体亚型5-HT1A拮抗剂WAY-100635的印迹聚合物被制备出来。
The resulting MIP P(WAY) was evaluated as an affinity matrix in the screening of serotonin receptor antagonists with known affinities for the native receptor.
结果产物MIP P(WAY) 在筛选与自然受体有亲和力的5-羟色胺受体拮抗剂中被评价为一种亲和基质。
Rough correlations in affinity between the synthetic P(WAY) and native receptor 5-HT1A were found. These findings provide some support for the analogy between MIPs and native receptors and their possible use as surrogates.
已经发现了合成P(WAY)和天然受体5-HT1A间亲和力的基本联系。这些发现结果为类推MIPs和天然受体及其可能代用品间关系提供了一些支持。
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